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Antifungal composition for external use being retentive in stratum corneum

a technology of antifungal composition and antifungal agent, which is applied in the direction of biocide, drug composition, aerosol delivery, etc., can solve the problems of insufficient penetration into the epidermal stratum corneum of antifungal agents, difficult to increase their solubility when incorporated in the base, and high affinity of antifungal agents for keratin. , to achieve the effect of enhanced penetration into the epidermal stratum corneum of said antifungal

Inactive Publication Date: 2000-01-25
TOKO YAKUHIN IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

More particularly, it has been found that in the preparation of compositions for external use containing as an active ingredient an antifungal agent having a high affinity for keratin, by incorporating with methyl salicylate, glycol salicylate, crotamiton, peppermint oil or menthol, which can dissolve said antifungal agents well and shows a good penetration into the stratum corneum, the penetration into the epidermal stratum corneum of said antifungal agents is enhanced, and further said antifungal agents are more tightly bound to the components of the epidermal stratum corneum, and fixed thereon.

Problems solved by technology

However, these antifungal agents having a high affinity for keratin are not readily soluble, and it is difficult to increase their solubility when incorporated in the base.
As a result, the penetration into the epidermal stratum corneum of these agents is not sufficient so as to form an antifungal composition for external use which is retentive in the stratum corneum using a high affinity for keratin of the active antifungal agent per se at the maximum.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 2 (

Ointment)

An ointment is prepared by the following formulation.

To plastibase is added a solution of ketoconazole in crotamiton and glycol salicylate which is prepared by warming at about 70 to 80.degree. C., and the mixture is well stirred and kneaded to give an ointment.

example 3 (

Ointment)

An ointment is prepared by the following formulation.

Polyethylene glycol 4000 is dissolved by warming on a water bath and thereto is added a solution of lanoconazole in crotamiton and polyethylene glycol 400, which is prepared by warming at about 70 to 80.degree. C., and the mixture is well stirred and, thereafter, cooled and kneaded until it becomes semisolid to give an ointment.

example 4 (

Ointment)

An ointment is prepared by the following formulation.

White vaseline is dissolved by warming on a water bath and thereto is added a solution of bifonazole in peppermint oil, isopropyl myristate and glycerin monostearate, which is prepared by warming at about 70 to 80.degree. C., and the mixture is well stirred and, thereafter, cooled and kneaded until it becomes semisolid to give an ointment.

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PUM

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Abstract

PCT No. PCT / JP95 / 00773 Sec. 371 Date Jan. 5, 1996 Sec. 102(e) Date Jan. 5, 1996 PCT Filed Apr. 19, 1995 PCT Pub. No. WO95 / 30440 PCT Pub. Date Nov. 16, 1995An antifungal composition for external use being retentive in the stratum corneum containing as an active ingredient an antifungal agent having a high affinity for keratin, wherein the penetration into the stratum corneum of said antifungal agent is enhanced and the retentivity thereof is improved, which comprises incorporating one or more oily liquid substances selected from the group consisting of methyl salicylate, glycol salicylate, crotamiton, and peppermint oil or menthol.

Description

The present invention relates to an antifungal composition for external use containing as an active ingredient an antifungal agent having a high affinity for keratin. More particularly, the present invention relates to an antifungal composition for external use being retentive in the stratum corneum, which contains one or more oily liquid substances selected from the group consisting of methyl salicylate, glycol salicylate, crotamiton, and peppermint oil or menthol, in order to enhance the penetration into the stratum corneum of the active antifungal agent having a high affinity for keratin, by which said antifungal agent is more retentive in the stratum corneum.In superficial mycosis, fungi invade mainly into the epidermal stratum corneum, and grow therein. Thus, in order to exhibit excellent pharmacological activities in the treatment of superficial mycosis, antifungal agents should stay in a high concentration in the infected epidermal stratum corneum for a prolonged time, in add...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K8/92A61K31/137A61K47/16A61K47/14A61K47/10A61K47/18A61K47/44A61K31/44A61K31/4174A61K31/4178A61K31/4164A61K31/496A61K31/5375A61K9/00A61K8/34A61K8/37A61K8/42A61K9/06A61K9/08A61K31/50A61K47/08A61K47/22A61K47/46A61P31/00A61P31/10A61Q17/00
CPCA61K8/34A61K8/37A61K8/375A61K8/42A61K8/922A61K9/0014A61K31/137A61K31/4174A61K31/4178A61K31/44A61K31/496A61K31/5375A61K47/10A61K47/14A61K47/18A61K47/44A61Q17/005Y10S514/912A61P31/00A61P31/10
Inventor KAMISHITA, TAKUZOMIYAZAKI, TAKASHI
Owner TOKO YAKUHIN IND CO LTD
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